Please use this identifier to cite or link to this item: http://www.repositorio.ufop.br/handle/123456789/11077
Title: Design and synthesis of new benzophenone derivatives with in vivo anti-inflammatory activity through dual inhibition of edema and neutrophil recruitment.
Authors: Januário, Jaqueline Pereira
Souza, Thiago Belarmino de
Lavorato, Stefânia Neiva
Maiolini, Tatiane Cristina Silva
Domingos, Olívia da Silva
Zanin, João Luiz Baldim
Folquitto, Laís Regina dos Santos
Soares, Marisi Gomes
Paula, Daniela Aparecida Chagas de
Dias, Danielle Ferreira
Santos, Marcelo Henrique dos
Keywords: Molecular docking
Hydrazinothiazole
Tiosemicarbazone
Ear edema
Structure activity relationship
Issue Date: 2018
Citation: JANUÁRIO, J. P. et al. Design and synthesis of new benzophenone derivatives with in vivo anti-inflammatory activity through dual inhibition of edema and neutrophil recruitment. Molecules, v. 23, n. 8, p. 1-23, jul. 2018. Disponível em: <https://www.mdpi.com/1420-3049/23/8/1859>. Acesso em: 7 mar. 2019.
Abstract: A series of novel benzophenone derivatives containing a thiazole heterocyclic nucleus were designed by molecular hybridization. Molecular docking studies have demonstrated the inhibitory potential of the designed compounds against cyclooxygenase (COX) isoenzymes. These compounds were synthesized, characterized, and evaluated for their anti-inflammatory properties by the croton oil-induced ear edema assay to examine their effect on both prostaglandin (PG) production and neutrophils recruitment. The thiazole derivatives displayed a potent effect in terms of reducing ear edema. The analysis suggested that the presence of 4-phenyl-2-hydrazinothiazole and the absence of C40 -OCH3 on the benzophenone derivative structure are strongly related to the inhibition of PG production. In addition, the derivatives 2e, 3a and 3c concomitantly inhibit PG production and neutrophil recruitment, which may be a mechanism of action better than of common NSAIDs due to their inability to inhibit the neutrophil recruitment. Thus, these compounds can be considered as potential lead compounds toward the development of new anti-inflammatory drugs with an innovating mechanism of action
URI: http://www.repositorio.ufop.br/handle/123456789/11077
ISSN: 1420-3049
metadata.dc.rights.license: This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/) wich permits copy and redistribute the material in any medium or format provided the original work is properly cited. Fonte: o próprio artigo.
Appears in Collections:DEFAR - Artigos publicados em periódicos

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